Pilocarpine (CID 5910) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(37)
 
 
Inactive(350)
 
 
Inconclusive(21)
 
 
Unspecified(66)
 
 
Top Targets:
p450(11)
 
 
 
 
 
7TM GPCR Srx(10)
 
 
 
PIKKc TOR(8)
 
 
Pyr redox dim(8)
 
 
 
Tubulin-bindi..(7)
 
 
 
BioAssay Types:
Confirmatory(281)
 
 
 
 
Literature(149)
 
 
 
 
 
Screening(14)
 
 
BioActivity Types:
Potency(259)
 
 
 
 
IC50(9)
 
 
Ki(7)
 
 
EC50(3)
 
 
 
Kd(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 268    Data Row: 474   Total Pages: 10   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103177090]
Ki 0.026Binding affinity against muscarinic acetylcholine receptor from rat brain crude membrane, using [3H]OXO-M (oxotremorine) as the radioligand. [AID142349, Type: Literature]
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2
[SID103177090]
IC50 0.067In vitro inhibition of [3H]Oxo-Mas binding to M1 and M4 receptors in rat brain homogenate. [AID142501, Type: Literature]
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3
[SID103177090]
IC50 0.068Binding affinity against muscarinic receptor in rat brain membranes using oxotremorine-M as ligand [AID225548, Type: Literature]
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4
[SID103177090]
IC50 0.08Ability to displace [3H]cis--2-methyl-5-((dimethylamino)methyl)-1,3-di oxolane from muscarinic acetylcholine receptor in rat cortical tissue. [AID141540, Type: Literature]
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5
[SID103177090]
Ki 0.0829Inhibition of [3H]OXO-M binding against muscarinic acetylcholine receptor in rat brain membranes [AID142081, Type: Literature]
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6
[SID103177090]
IC50 0.96Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue. [AID141554, Type: Literature]
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7
[SID103177090]
ED50 1Tested in vitro for agonistic effect on Muscarinic acetylcholine receptor of guinea pig ileum [AID141133, Type: Literature]
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8
[SID103177090]
Ki 1.01Inhibition of [3H]QNB binding against muscarinic acetylcholine receptor in rat brain. [AID142079, Type: Literature]
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9
[SID103177090]
Ki 1.11The compound was tested for inhibition of [3H]NMS binding against muscarinic acetylcholine receptor in rat brain [AID142078, Type: Literature]
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10
[SID103177090]
Ki 3.1Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M1, using [3H]- pirenzepine, a radioligand displacement assay in rat hippocampal membranes [AID141718, Type: other]
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11
[SID103177090]
Ki 3.67Binding affinity against muscarinic acetylcholine receptor from rat brain crude membrane, using [3H]-NMS (N-Methylscopolamine) as the radioligand. [AID142348, Type: Literature]
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12
[SID103177090]
IC50 4.43Compound was evaluated for the displacement of the muscarinic QNB in a genetically transformed rat cell line (m1c2) transfected with cloned m1 receptors (m1-QNBm1c2) [AID142712, Type: other]
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13
[SID103177090]
EC50 6.9Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line [AID141319, Type: Literature]Muscarinic acetylcholine receptor M [gi:408359949]
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14
[SID103177090]
IC50 7.6Inhibition of [3H](R)-QNB binding to muscarinic receptor in rat brain membranes [AID142711, Type: other]Muscarinic acetylcholine receptor M [gi:113121]
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15
[SID103177090]
IC50 7.6Inhibition of [3H](R)-QNB binding to muscarinic receptor in rat brain membranes [AID142711, Type: other]Muscarinic acetylcholine receptor M [gi:113121]
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16
[SID103177090]
IC50 7.6Inhibition of [3H](R)-QNB binding to muscarinic receptor in rat brain membranes [AID142711, Type: other]Muscarinic acetylcholine receptor M [gi:113121]
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17
[SID103177090]
IC50 7.6Inhibition of [3H]-(R)-QNB binding to muscarinic receptors of rat brain membranes. [AID104017, Type: Literature]Muscarinic acetylcholine receptor M [gi:113121]
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18
[SID103177090]
IC50 7.6Inhibition of [3H]-(R)-QNB binding to muscarinic receptors of rat brain membranes. [AID104017, Type: Literature]Muscarinic acetylcholine receptor M [gi:113121]
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19
[SID103177090]
IC50 7.6Inhibition of [3H]-(R)-QNB binding to muscarinic receptors of rat brain membranes. [AID104017, Type: Literature]Muscarinic acetylcholine receptor M [gi:113121]
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20
[SID103177090]
IC50 7.6Inhibition of specific [3H](R)-QNB binding to Muscarinic acetylcholine receptor in rat brain membranes [AID142488, Type: Literature]
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21
[SID11113352]
Potency 7.9433qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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22
[SID11113352]
Potency 7.9433qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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23
[SID103177090]
EC50 8.792Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor [AID142284, Type: Literature]
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24
[SID103177090]
IC50 8.8Compound was evaluated for the displacement of the muscarinic QNB in rat heart homogenate containing the pharmacologic M2 receptor (M2-QNB heart) [AID142864, Type: other]
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25
[SID103177090]
Ki 9.8Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M2, using [3H]- N-methyl-scopolamine, a radioligand displacement assay in rat heart membranes [AID142945, Type: other]
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26
[SID103177090]
Kd 10Central presynaptic activity as effect on electrically evoked acetylcholine release from rat hippocampal slices (M2 model) [AID140934, Type: Literature]Muscarinic acetylcholine receptor M [gi:12643977]
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27
[SID103177090]
Kd 10Central presynaptic activity as effect on electrically evoked acetylcholine release from rat hippocampal slices (M2 model) [AID140934, Type: Literature]Muscarinic acetylcholine receptor M [gi:12643977]
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28
[SID11113352]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C9 [AID883, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:13699818]
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29
[SID11113352]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C9 [AID883, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:13699818]
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30
[SID11113352]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C9 [AID883, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:13699818]
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31
[SID11113352]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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32
[SID11113352]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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33
[SID11113352]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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34
[SID26751548]
Potency 26.6795Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS [AID504845, Type: confirmatory]regulator of G-protein signaling 4 [Homo sapiens] [gi:86301163]
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35
[SID26751548]
Potency 26.6795Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS [AID504845, Type: confirmatory]regulator of G-protein signaling 4 [Homo sapiens] [gi:86301163]
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36
[SID26751548]
Potency 26.6795Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS [AID504845, Type: confirmatory]regulator of G-protein signaling 4 [Homo sapiens] [gi:86301163]
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37
[SID11113352]
 Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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38
[SID11113352]
 Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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39
[SID11113352]
 Cytochrome panel assay with activity outcomes [AID1851_3, Type: other]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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40
[SID11113352]
 Cytochrome panel assay with activity outcomes [AID1851_3, Type: other]cytochrome P450, family 3, subfamily A, polypeptide 4 [Homo sapiens] [gi:13435386]
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41
[SID11113352]
 Cytochrome panel assay with activity outcomes [AID1851_5, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:13699818]
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42
[SID11113352]
 Cytochrome panel assay with activity outcomes [AID1851_5, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 9 [Homo sapiens] [gi:13699818]
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43
[SID11113352]
 qHTS Assay for Tau Filament Binding [AID596, Type: confirmatory]Microtubule-associated protein tau [Homo sapiens] [gi:92096784]
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44
[SID11113352]
 qHTS Assay for Tau Filament Binding [AID596, Type: confirmatory]Microtubule-associated protein tau [Homo sapiens] [gi:92096784]
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45
[SID103177090]
 Compound was evaluated for dissociation constant (KA), determined from potency against Muscarinic acetylcholine receptor M3 in an isolated tissue assay (guinea pig trachea) [AID141074, Type: other]
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46
[SID103177090]
 Conditioned avoidance responding in rat after subcutaneous administration (1 mg/kg); expressed as avoidance response/response failure; 18/21 [AID169191, Type: Literature]
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47
[SID103177090]
 In vitro for its ability to displace [3H]NMS from muscarinic acetylcholine receptor in rat cortical homogenates [AID142097, Type: Literature]
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48
[SID103177090]
 In vitro displacement of [3H]OXO-M from muscarinic acetylcholine receptor in rat cortical homogenates [AID142098, Type: Literature]
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49
[SID103177090]
 In vitro binding affinity against muscarinic acetylcholine receptor from rat cortical homogenates using [3H]N-methylscopolamine as radioligand [AID142209, Type: Literature]
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50
[SID103177090]
 In vitro binding affinity against muscarinic acetylcholine receptor from rat cortical homogenates using [3H]oxotremorine-M radioligand [AID142210, Type: Literature]
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